Bleomycinum

Блеомицин Constitutional formula

The description is actual on 19.09.2015

  • Latin name: Bleomycinum
  • ATH code: L01DC01
  • Chemical formula: C55H84N17O21S3
  • CAS code: 41138-54-9

Chemical name

(3-{ [(2 ′-{ (5S,8S,9S,10R,13S)-15-{ 6-Amino-2-[(1S) - 3-amino-1-{ [(2S) - 2,3-diamino-3-oxopropyl] amine } - 3 oxopropyl] - 5-methylpyrimidine-4-silt }-13-[{ [(2R,3S,4S,5S,6S)-3-{ [(2R,3S,4S,5R,6R)-4 (karbamoiloksa) - 3,5-digidroksi-6-(hydroxymethyl) tetrahydro-2H-pyrane-2-silt] oks } - 4,5-digidroksi-6-(hydroxymethyl) tetrahydro-2H-pyrane-2-silt] oks } (1H-imidazole-5-silt) marked] - 9-gidroksi-5-[(1R)-1-a hydroxyethyl] -8,10-диметил-4,7,12,15-тетраоксо-3,6,11,14-тетраазапентадец-1-ил}-2,4-би-1,3-тиазол-4-ил) a carbonyl] amine } spent on drink) (dimethyl) sulphonium

Chemical properties

Bleomycinum – a glycopeptide antibiotic which is synthesized by bacteria of Streptomyces verticillus, cytostatics. Substance represents mix from various glycopeptide antibiotics, A2, B2 fractions and others.

Means is synthesized in the form of sulfate or a hydrochloride. The molecular mass of connection = 1415, 5 grams on mol. Let out medicine in the form of liquids for injection introduction or introduction to cavities.

Pharmacological action

Antineoplastic.

Pharmacodynamics and pharmacokinetics

Substance causes fragmentation of protein and nucleic acids, in particular deoxyribonucleic acid in cancer cells. At interaction with DNA means leads to a rupture of one or two chains of amino-acid sequences and to education of free radicals. It occurs owing to oxidation of the DNK-bleomitsin-dvukhvalentnoye complex iron. Medicine influences cells in a mitosis phase, substance shows the greatest activity in relation to cells in the phase G2. Effect of drug dozozavisy. Due to these frequent introduction of low dosages or carrying out long infusions is recommended.

Medicine rather poorly influences processes of a hemopoiesis in marrow, cellular and humoral immunity practically does not oppress.

Drugs of Bleomycinum exert negative toxic impact on lungs. At early stages diffusion capacity of lungs decreases, there are rattles, the pneumonitis develops. Further there can be a pneumosclerosis, blackouts on roentgenoscopy, death cases are known.

Medicine possesses the greatest efficiency at early stages. Metastasises are a little sensitive to influence of this substance.

When using medicine for treatment of tumors of ovaries or a lymphogranulomatosis of improvement in a condition of the patient come in 14 days of use, at a planocellular carcinoma – in 21 days.

Long instillation at a pleural exudate considerably reduces probability of development of recurrence (to 64%).

Ames's test showed that substance does not possess mutagen activity, however some laboratory and clinical data show the return. Also drug can has teratogenic and cancerogenic influence on the person.

At intra belly and intrapleural use the level of system absorption reaches 45%. Medicine collects in cells of a tumor, lungs, to a lesser extent – in kidneys, lymph nodes, a peritoneum, in insignificant quantity – in hemopoietic fabrics. Extent of linkng of substance with proteins of plasma extremely low, less than 1%.

Means is exposed to reactions of a metabolism during splitting in fabrics and bodies by means of specific enzymes. If the clearance of creatinine reaches more than 35 ml a minute, then the substance elimination half-life makes 115 minutes of a blood plasma, at KK less than 35 ml a minute occur the exponential growth of this indicator. At patients with normally functioning kidneys about 65% of substance are removed in not changed view with urine.

Indications to use

Medicine is appointed, as a rule, in combination with other cytostatics or radiation therapy.

Means is used:

  • for treatment of a planocellular carcinoma cutaneum;
  • at a cancer of a penis or vulva (neck of uterus);
  • for treatment of malignant new growths of a neck and the head;
  • to patients with a cancer of a gullet or lungs;
  • at germinogenny tumors of an ovary;
  • patient with cancer of a kidney;
  • at a teratocarcinoma of the first and second stage (combine with vinblastine);
  • for treatment of hodzhkinsky or nekhodzhkinsky lymphoma;
  • at a reticulosarcoma, a glioma and Kaposha's sarcoma (against AIDS);
  • for prevention or treatment of a pleural exudate.

Contraindications

Bleomycinum is contraindicated to use:

  • to patients with the expressed breath dysfunctions;
  • at fibrosis of pulmonary fabric;
  • the patient with serious violations in work of kidneys (clearance of creatinine less than 35 ml a minute);
  • at liver diseases;
  • to pregnant women;
  • at the heavy course of cardiovascular diseases;
  • in the period of a lactation;
  • at an ataxy teleangiectasia;
  • at an allergy to active ingredient;
  • to patients at the age of more than 80 years.

It is recommended to be careful:

  • if earlier it was carried out beam or chemotherapy;
  • at acute viral or infectious diseases;
  • aged till 18 flyings.

Side effects

During treatment can develop:

  • vomiting, nausea, diarrhea, appetite loss;
  • discoloration and thickness of skin, an itch and an enanthesis, outgrowths on the ends of fingers, palms and joints, emergence of dark strips on skin, swelling of fingers, reddenings on finger-tips;
  • seldom – disturbances in work of kidneys, an ischuria, an urodynia, a vulvitis, a pollakiuria;
  • decrease in lung volume, pneumonitis, fibrosis pulmonary, rattles, an otdyshka and a severe cough (remain within 30 days after the therapy termination);
  • fragility of nails, hair loss, structural changes of a nail plate;
  • weight reduction of the patient, fibrinferments, phlebitis, consecutive infections, conjunctivitis;
  • seldom – a stroke, Reynaud's syndrome, a myocardial infarction, cerebral arteritis, a trombotichesky mikroangiopatiya, bleedings, an angialgiya;
  • seldom – increase of level of enzymes of a liver, stomatitises;
  • small tortoiseshell and other allergic reactions, acute anaphylaxis;
  • seldom – increase of the ABP, fervescence, fever, a fever, stertorozny breath, confusion of consciousness and a disorientation.

At intrapleural introduction often there is pain in the field of a tumor, various local pains.

Bleomycinum, application instruction (Way and dosage)

The mode of dosing is set in an individual order. The dosage and the scheme of treatment depend on a stage of a disease, a condition of the patient, drugs in parallel used.

Means is appointed intramusculary, intravenously, subcutaneously, vnutriarterialno, entered into cavities.

The standard one-time dosage makes 15 mg of means, medicine is entered slowly, intravenously, infusion lasts at least 15 minutes. Substance is dissolved in solution of glucose or sodium chloride.

At intramuscular and hypodermic use introduction of 30 mg of means is recommended (as much as possible).

Overdose

Probability of overdose low because medicine is used in the conditions of a hospital.

Interaction

Cisplatinum increases toxicity of this drug.

If during the general anesthesia oxygen is used, then Bleomycinum increases probability of development of pneumotoxic action.

At a combination to the drugs having myelotoxic or pneumotoxic effect the risk of emergence of side reactions increases.

Other antineoplastic means and use of radiation therapy increase toxicity of medicine for marrow.

Vincristinum increases efficiency of treatment by means.

Special instructions

Administration of drug has to is made by pilot medical personnel.

During therapy passing by this drug it is necessary to make periodic control of function of kidneys, a respiratory organs, a liver, to do a thorax X-ray.

With extra care substance appoint to children, especially premature and newborn (only according to vital indications).

If during treatment by means at the patient arose dispnoe or a severe cough, discolorations and structures of skin, then therapy the patient is recommended to stop and appoint antibiotics and glucocorticosteroids.

Temperature increase in 5 hours after an injection or infusion of medicine assumes that it is necessary to reduce a one-time dosage of drug.

During treatment of women of childbearing age it is necessary to use reliable ways of protection against undesirable pregnancy and STD.

During researches it was revealed that long 24-hour infusion of means reduces probability of development of side reactions from respiratory system, however increases risk of toxic impact on mucous membranes and integuments a little.

Elderly

It is necessary to observe extra care at treatment of patients 80 years are more senior.

At pregnancy and a lactation

Pregnant women cannot accept Bleomycinum. Medicine possesses teratogenic and embriotoksichesky action.

During treatment by this substance breastfeeding needs to be interrupted.

Drugs in which contains (Analogues of Bleomycinum)

Substance is a part: Vero-Bleomitsin, Blenamaks, Bleomitsetina a hydrochloride for injections of 0,005 g, Bleotsin, Bleomitsetina a hydrochloride, Bleomitsin-RONTs.

About Bleomycinum

About medicine generally good, side reactions are shown not more often than it is noted in the instruction.

Some About Bleomycinum drugs:

  • "… Means was appointed to my father. During treatment at it pressure began to rise and to press in heart, the otdyshka appeared. Made the cardiogram and revealed disturbances in work of cardiovascular system. Treatment had to be stopped and some time to be recovered. Then Bleomycinum was not appointed any more to avoid recurrence";
  • "… Bleomycinum injections already a lot of time are given to my brother. Transfers treatment well, it practically has no side reactions, but pains passed, is on the mend. But here it seems to me, all individually, someone can have also absolutely other reaction".
Section: Active ingredients
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